LEI110
Based on 1 publication(s) in Google Scholar
LEI110 is a pan-inhibitor of the HRASLS family and an inhibitor of AP-2α, with a Ki of 20 nM against PLA2G16. LEI110 exhibits inhibitory activity against PLA2G16, HRASLS2, RARRES3 and iNAT, with pIC50 values of 7.0, 6.8, 6.8 and 7.6, respectively. LEI110 binds to the active site of PLA2G16, reduces intracellular arachidonic acid levels, and attenuates oleic acid-induced lipolysis. LEI110 stabilizes AP-2α, impairs its DNA-binding ability, inhibits the transcription of DNA damage repair genes, induces the accumulation of oxidative DNA damage, suppresses cell proliferation and clonogenicity, and sensitizes HCC cells to DNA-damaging agents. LEI110 can be used in research related to obesity, fatty liver disease, the common cold and hepatocellular carcinoma.
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- Pureté : 99.72%
- CAS No.: 2313525-90-3
- Formule: C25H23F3N2O3
- Masse moléculaire:456.46
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) LEI110
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Activité biologique
Description
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HRASLS2 6.8 (pIC50) |
PLA2G16 20 nM (Ki) |
RARRES3 6.8 (pIC50) |
iNAT 7.6 (pIC50) |
PLA2G16 7 (pIC50) |
AP-2α |
In Vitro
LEI110 (0.001-100 μM) potently inhibits PLA2G16 (pIC50 = 7.0) and other HRASLS family members (HRASLS2, RARRES3, iNAT) in the cytosolic proteome of overexpressing HEK293T cells, and acts as a selective pan-inhibitor of the HRASLS thiol hydrolase family[1].
LEI110 potently inhibits the enzymatic activity of recombinant human PLA2G16 in vitro, with a Ki of 20 nM[1].
LEI110 (10 μM; 4-8 h) reduces PLA2G16-induced arachidonic acid levels in U2OS cells overexpressing PLA2G16 in a time-dependent manner, with nearly complete inhibition observed after 8 h[1].
LEI110 (10 μM; 24 h pre-incubation followed by co-incubation with 100 μM Oleic Acid (HY-N1446) for 24 h) inhibits oleic acid-induced lipolysis and lipid droplet accumulation in human HepG2 cells[1].
LEI110 (1 h treatment) stabilizes the AP-2α protein in human hepatocellular carcinoma cell line HEP3B, confirming a direct binding interaction between LEI110 and AP-2α[2].
LEI110 (2-128 μM) significantly reduces the viability of human hepatocellular carcinoma cell lines HEP3B, Huh7, MHCC-97H and SNU387 in a dose-dependent manner[2].
LEI110 (administered for 4 consecutive days) inhibits the proliferation of HEP3B human hepatocellular carcinoma cells over a 4-day treatment cycle[2].
LEI110 (20 μM; 10 days) potently inhibits the colony-forming ability of HEP3B human hepatocellular carcinoma cells, reducing the colony formation rate to approximately 25% of that in the control group[2].
LEI110 (0-48 hours) inhibits the expression of DDR genes NUDT1, PARP1, TOP2A and POLD1 in human hepatocellular carcinoma cells in a time-dependent manner, with significant down-regulation detectable as early as 12 hours after treatment[2].
LEI110 (20 μM) induces DNA damage in human hepatocellular carcinoma cell line HEP3B, and the proportion of γH2AX-positive cells doubles compared with that of the control group[2].
LEI110 (3.125-50 μM; 72 hours) exhibits strong synergistic cytotoxicity with the DNA-damaging agents H2O2, hydroxyurea, TH5487 and cisplatin in human hepatocellular carcinoma HEP3B cells, with the highest synergy score (approximately 11) observed in combination with H2O2[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human HCC HEP3B cells
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Concentration:3.125-50 μM (LEI110); 32-1024 μM (H2O2)
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Incubation Time:72 hours
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Result:Exhibited strong synergistic effects with all tested DNA-damaging reagents.
Achieved the highest synergy score (ZIP method) of ~11 with H2O2, followed by ~7 with TH5487, ~6 with hydroxyurea, and ~4 with cisplatin.
Showed enhanced cytotoxicity with increasing concentrations of both LEI110 and H2O2 in combined treatment.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Healthy mice[2]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection (i.p.); single administration; 24 h
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Result:Caused no observable behavioral abnormalities or histological liver alterations.
Chemical Information
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CAS No. 2313525-90-3
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Appearance Solid
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Masse moléculaire 456.46
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Formule C25H23F3N2O3
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Color Light yellow to yellow
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SMILES
O=C(NCCC1=CC=C(OC2=NC=C(C(F)(F)F)C=C2)C=C1)C(CCCC3=CC=CC=C3)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (219.08 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Zhou J, et al. Activity-Based Protein Profiling Identifies α-Ketoamides as Inhibitors for Phospholipase A2 Group XVI. ACS chemical biology. 2019 Feb 15;14(2):164-169. [Content Brief]
[2]. Wang C, et al. Macroscopic inhibition of DNA damage repair pathways by targeting AP-2α with LEI110 eradicates hepatocellular carcinoma. Communications Biology. 2024;7:342. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1908 mL | 10.9539 mL | 21.9077 mL | 54.7693 mL |
| 5 mM | 0.4382 mL | 2.1908 mL | 4.3815 mL | 10.9539 mL | |
| 10 mM | 0.2191 mL | 1.0954 mL | 2.1908 mL | 5.4769 mL | |
| 15 mM | 0.1461 mL | 0.7303 mL | 1.4605 mL | 3.6513 mL | |
| 20 mM | 0.1095 mL | 0.5477 mL | 1.0954 mL | 2.7385 mL | |
| 25 mM | 0.0876 mL | 0.4382 mL | 0.8763 mL | 2.1908 mL | |
| 30 mM | 0.0730 mL | 0.3651 mL | 0.7303 mL | 1.8256 mL | |
| 40 mM | 0.0548 mL | 0.2738 mL | 0.5477 mL | 1.3692 mL | |
| 50 mM | 0.0438 mL | 0.2191 mL | 0.4382 mL | 1.0954 mL | |
| 60 mM | 0.0365 mL | 0.1826 mL | 0.3651 mL | 0.9128 mL | |
| 80 mM | 0.0274 mL | 0.1369 mL | 0.2738 mL | 0.6846 mL | |
| 100 mM | 0.0219 mL | 0.1095 mL | 0.2191 mL | 0.5477 mL |
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